Cyclo(Arg-Gly-Asp-D-Phe-Val)
Cyclo(Arg-Gly-Asp-D-Phe-Val) (Cyclo(RGDfV)) is an integrin αvβ3 inhibitor. Cyclo(Arg-Gly-Asp-D-Phe-Val) has antitumor activity. Cyclo(Arg-Gly-Asp-D-Phe-Val) can be used for the research of acute myeloid leukemia.
For research use only. We do not sell to patients.
- CAS No.: 137813-35-5
- Formula: C26H38N8O7
- Molecular Weight:574.63
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
αvβ3[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
3.25 x 10-7 M
Compound: 6, c(RGDfV)
|
Displacement of [125I]echistatin from human integrin alpha5beta3 expressed in human A549 cells by binding assay
Displacement of [125I]echistatin from human integrin alpha5beta3 expressed in human A549 cells by binding assay
|
[PMID: 21349709] |
| A549 | IC50 |
3.25 x 10-1 μM
Compound: 6, c(RGDfV)
|
Displacement of [125I]echistatin from human integrin alpha5beta3 expressed in human A549 cells by binding assay
Displacement of [125I]echistatin from human integrin alpha5beta3 expressed in human A549 cells by binding assay
|
[PMID: 21349709] |
| HUVEC | IC50 |
0.53 μM
Compound: CycloRGDfV
|
Inhibition of HUVEC migration after 4 hrs
Inhibition of HUVEC migration after 4 hrs
|
[PMID: 19081719] |
| HUVEC | IC50 |
3.1 μM
Compound: CycloRGDfV
|
Inhibition of FGF-induced HUVEC proliferation after 48 hrs
Inhibition of FGF-induced HUVEC proliferation after 48 hrs
|
[PMID: 19081719] |
| HUVEC | IC50 |
4.5 μM
Compound: CycloRGDfV
|
Inhibition of VEGF-induced HUVEC proliferation after 48 hrs
Inhibition of VEGF-induced HUVEC proliferation after 48 hrs
|
[PMID: 19081719] |
| HUVEC | IC50 |
9.6 μM
Compound: c[RGDfV]
|
Inhibition of alphavbeta3 integrin-mediated cell adhesion in HUVEC on vitronectin coated plate after 30 mins
Inhibition of alphavbeta3 integrin-mediated cell adhesion in HUVEC on vitronectin coated plate after 30 mins
|
[PMID: 20055426] |
| K562 | IC50 |
0.68 μM
Compound: c (RGDfV)
|
Inhibition of adhesion of K562 cells expressing alphaVbeta3 integrin receptor to vitronectin
Inhibition of adhesion of K562 cells expressing alphaVbeta3 integrin receptor to vitronectin
|
[PMID: 16722662] |
| K562 | IC50 |
34.7 μM
Compound: c[RGDfV]
|
Inhibition of alpha5beta1 integrin-mediated cell adhesion in human K562 cells on fibronectin coated plate after 30 mins
Inhibition of alpha5beta1 integrin-mediated cell adhesion in human K562 cells on fibronectin coated plate after 30 mins
|
[PMID: 20055426] |
| K562 | IC50 |
34.7 μM
Compound: cyclo-Arg-Gly-Asp-D-Phe-Val
|
Antagonist activity at alpha5beta1 integrin in human K562 cells assessed as inhibition of fibronectin-mediated cell adhesion after 30 mins by fluorescence assay
Antagonist activity at alpha5beta1 integrin in human K562 cells assessed as inhibition of fibronectin-mediated cell adhesion after 30 mins by fluorescence assay
|
[PMID: 24973662] |
| M21 | IC50 |
0.6 μM
Compound: c (RGDfV)
|
Inhibition of integrin alphavbeta3 mediated cell adhesion of human M21 cells to vitronectin
Inhibition of integrin alphavbeta3 mediated cell adhesion of human M21 cells to vitronectin
|
[PMID: 16982193] |
| WM-115 | IC50 |
0.5 μM
Compound: c-(-Arg-Gly-Asp-D-Phe-Val-)
|
Binding affinity to integrin in human WM-115 cells after 30 mins by immobilized vitronectin-based competitive cell adhesion assay
Binding affinity to integrin in human WM-115 cells after 30 mins by immobilized vitronectin-based competitive cell adhesion assay
|
[PMID: 23387527] |
Cyclo(Arg-Gly-Asp-d-Phe-Val) (Cyclo(RGDfV)) (35 nM, 4-24 h) disruptes the adhesion and migration between the tumor cells and the matrix, induces the leukemia cells to leave the protective microenvironment and increases their sensitivity to cell cycle-dependent agents[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV4–11 cells
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Concentration:35 nM
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Incubation Time:24 h
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Result:Affected the leukemia cell cycle, decreased the G0/G1 phase of leukemia cells in the 3D and 2D culture systems and increased the S phase of leukemia cells in the 3D and 2D culture systems.
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Cell Line:MV4–11 cells
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Concentration:35 nM
-
Incubation Time:24 h
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Result:Increased the apoptosis rates.
Chemical Information
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CAS No. 137813-35-5
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Molecular Weight 574.63
-
Formula C26H38N8O7
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Synonyms
Cyclo(RGDfV); C(RGDfV)
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Sequence Shortening
Cyclo(RGD-{d-Phe}-V)
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)